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Assay Detail

CHEMBL858096

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-2C adrenergic receptor (CHEMBL1916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Hodson SJ, Bishop MJ, Speake JD, Navas F, Garrison DT, Bigham EC, Saussy DL, Liacos JA, Irving PE, Gobel MJ, Sherman BW.
J Med Chem (2002) 45 : 2229 -2239
PubMed 12014961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.77 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70751 1 8.55
CHEMBL72768 1 8.25
CHEMBL72724 1 8.10
CHEMBL72441 1 8.05
CHEMBL540035 1 7.55
CHEMBL306792 1 7.00
CHEMBL74114 1 6.35
CHEMBL70634 1 6.10
CHEMBL71479 1 5.95
CHEMBL74467 1 5.70
CHEMBL72958 NS-49 1 5.70
CHEMBL544290 1 5.50
CHEMBL70740 1 5.20
CHEMBL302698 1 -
CHEMBL70563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70751 EC50 = 2.818 nM 8.55
CHEMBL72768 EC50 = 5.623 nM 8.25
CHEMBL72724 EC50 = 7.943 nM 8.10
CHEMBL72441 EC50 = 8.913 nM 8.05
CHEMBL540035 EC50 = 28.18 nM 7.55
CHEMBL306792 EC50 = 100.0 nM 7.00
CHEMBL74114 EC50 = 446.68 nM 6.35
CHEMBL70634 EC50 = 794.33 nM 6.10
CHEMBL71479 EC50 = 1122.02 nM 5.95
CHEMBL74467 EC50 = 1995.26 nM 5.70
CHEMBL72958 NS-49 EC50 = 1995.26 nM 5.70
CHEMBL544290 EC50 = 3162.28 nM 5.50
CHEMBL70740 EC50 = 6309.57 nM 5.20
CHEMBL302698 EC50 < 10000.0 nM -
CHEMBL70563 EC50 < 10000.0 nM -